Antholine W E, Petering D H, Saryan L A, Brown C E
Proc Natl Acad Sci U S A. 1981 Dec;78(12):7517-20. doi: 10.1073/pnas.78.12.7517.
The interaction of sulfur-containing ligands with complexes of Fe(II) bleomycin [Fe(II)Blm] was investigated by comparing DNA strand-scission activity with the structural characteristics of the complex. The bithiazole ring of excess Blm can form intermolecular complexes with Fe(II)Blm and with NO-Fe(II)Blm, and the bithiazole groups of CO-Fe(II)Blm interact with the metal center. This binding can be reversed by glutathione, CO-Fe(II)Blm binds to poly(dA-dT) . poly(dA-dT) via its bithiazole group to change the environment of the Fe2+ ion. Glutathione binds to the CO-Fe(II)Blm-poly(dA-dT) . poly(dA-dT) complex under conditions in which it stimulates DNA strand scission by Fe(II)Blm.
通过比较DNA链断裂活性与配合物的结构特征,研究了含硫配体与铁(II)博来霉素配合物[Fe(II)Blm]之间的相互作用。过量博来霉素的双噻唑环可与Fe(II)Blm和NO-Fe(II)Blm形成分子间配合物,而CO-Fe(II)Blm的双噻唑基团与金属中心相互作用。这种结合可被谷胱甘肽逆转,CO-Fe(II)Blm通过其双噻唑基团与聚(dA-dT)·聚(dA-dT)结合,从而改变Fe2+离子的环境。在谷胱甘肽刺激Fe(II)Blm导致DNA链断裂的条件下,谷胱甘肽与CO-Fe(II)Blm-聚(dA-dT)·聚(dA-dT)配合物结合。